Cancer Targeted Therapy

Dutacatib is inhibitor for SARS-CoV-2 3CL^pro and cathepsin K, which exhibits antiviral activity and ameliorates the cancer-induced bone diseases.

5’(R)-C-Methyl-3-deazauridine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc.

ZINC57632462 (ACA-6) is a non-covalent allosteric KRAS inhibitor. ZINC57632462 disrupts nucleotide exchange and inhibits RAS-effector interaction. ZINC57632462 can be used for the research of cancer.

GP130-IN-1 (compound 49) is a potent GP130 inhibitor with significant in vitro antitumor activity and higher selectivity than Bazedoxifene (HY-A0031). GP130-IN-1 induces ultrastructural changes in cells, causing cell cycle arrest in the G0/G1 phase in a time-dependent manner and triggering apoptosis and autophagy. GP130-IN-1 can be used in the study of triple-negative breast cancer.

NUAK1-IN-1 (Compound 9) is a NUAK1 (IC₅₀ of 5.012 nM) and CDK4 inhibitor. NUAK1-IN-1 can be used in cancer, neurodevelopmental disorders and Alzheimer's disease research.

Fmoc-PEG3-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

mmu-miR-5625-3p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.

mmu-miR-7117-5p inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.

rno-miR-702-3p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.

m-PEG20-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

GSK137 is an orally active, potent and selective B-cell lymphoma 6 (BCL6) inhibitor. GSK137 blocks the interaction between BCL6 and corepressors (e.g., SMRT), reducing the number of germinal center B cells. GSK137 is promising for research of autoimmune diseases such as systemic lupus erythematosus (SLE) and B-cell-related tumors such as diffuse large B-cell lymphoma.

MAIPGG is a bifunctional chelator and an intermediate in the synthesis of radionuclide drug conjugates (RDCs). MAIPGG can be for the radiolabeling of a variety of monoclonal antibodies with ^99mTc or ¹⁸⁶Re, which then can be used for radioimmunodetection and radioimmunotherapy of cancer.

H-Cit-Lys(ma-Lys(PEG16))-Tyr-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

(S)-IP-DK143 is a polymeric micellar formulation. (S)-IP-DK143 inhibits the proliferation of cervical cancer cells, induces ROS-mediated apoptosis, and triggers mitochondrial dysfunction. (S)-IP-DK143 activates the p38 MAPK signaling pathway, increases the phosphorylation level of p38. (S)-IP-DK143 can be used for the research of cervical cancer.

KDM2A/7-IN-1 is a lysine demethylase 2A (KDM2A) inhibitor with a human IC₅₀ of 11 nM. KDM2A/7-IN-1 requires co-factor 2-oxoglutarate (2OG) for binding and occupies the H3K36me2 substrate pocket via a dimethylated lysine 36-mimicking group. KDM2A/7-IN-1 represses E2F-regulated genes, induces epithelial-mesenchymal transition, DNA repair, and mTOR pathways in specific cells, and selectively inhibits proliferation of ALT-positive cancer cell lines. KDM2A/7-IN-1 can be used for the research of ALT-positive cancers.

hsa-miR-6830-3p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.

mmu-miR-222-3p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.

mmu-miR-669h-5p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.

mmu-miR-7671-3p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.

BRM/BRG1 ATP-IN-8 (Compound Cpd14) is an orally active BRG1/BRM ATPase domain inhibitor. BRM/BRG1 ATP-IN-8 exerts antitumor effects by disrupting aberrant chromatin remodeling in cancer cells, inducing apoptosis and growth arrest. BRM/BRG1 ATP-IN-8 is promising for research of BRG1/BRM-dependent malignancies, including hematological cancers, prostate cancer, breast cancer, and Ewing's sarcoma.